Larotrectinib sulfate (LOXO-101, ARRY-470)是一种可口服的、选择性的、ATP竞争性的原肌球蛋白受体激酶TRK的有效抑制剂。Larotrectinib 对TRKs的抑制作用可诱导细胞凋亡和G1细胞周期阻滞。 Information Larotrectinib (LOXO-101) sulfate Larotrectinib sulfate (LOXO-101, ARRY-470) is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK) . Larotrectinib inhibition of TRKs induces cellular apoptosis and G1 cell-cycle arrest. Targets TRK In vitro ARRY-470(LOXO-101) is a selective kinase inhibitor with nanomolar activity against TRKA, TRKB and TRKC but no other notable kinase inhibition below 1,000 nM. ARRY-470 does not inhibit proliferation of Ba/F3 cells expressing other oncogene targets (epidermal growth factor receptor (EGFR), ALK or ROS1) or of lung and colorectal cell lines that do not harbor an NTRK1 fusion. It induces cell-cycle arrest in G1 and apoptosis of KM12 cells. In vivo Early/sustained but not late/acute administration of ARRY-470(LOXO-101) markedly attenuates bone cancer pain and significantly blocks the ectopic sprouting of sensory nerve fibers and the formation of neuroma-like structures in the tumor bearing bone, but does not have a significant effect on tumor growth or bone remodeling. It has very limited ability crossing of the blood brain barrier. Cell Research(from reference) Cell lines：Ba/F3 cells Concentrations：10, 100, 1000 nM Incubation Time：5 h
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
Larotrectinib (LOXO-101) sulfate
CAS number：1223405-08-0 molecular formula：C21H22F2N6O2.H2SO4
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | 2-[4-(2-sulfonatoethyl)piperazine-1,4-diium-1-yl]ethanesulfonate | AC-30671 | LOXO-101 (sulfate) | MS-29743 | D11138 | LAROTRECTINIB SULFATE [ORANGE BOOK] | (4-methylphenyl)-boronic acid | EX-A1981A | (3S)-N-{5-[(2R)-2-(2,5-Difluorophenyl)pyrrolidin-1-yl] | ||
| CAS number | 1223405-08-0 | molecular formula | C21H22F2N6O2.H2SO4 |
| molecular weight | 526.51 g/mol | Exact mass | ≥98% |
| PSA | 169.000 Ų | logp | 1.374 |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
No safety information yet
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
